Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 1999, Vol. 10 ›› Issue (4): 207

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Preparation of 11C labelled tamoxifen

LIU Ning1, DING Yu-Shin2   

  1. 1 Key Laboratory of Radiation Physics and Technology of Ministry of Education of China, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064;
    2 Department of Chemistry, Brookhaven National Laboratory, Upton, NY11973, U.S.A
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LIU Ning, DING Yu-Shin. Preparation of 11C labelled tamoxifen.Nuclear Science and Techniques, 1999, 10(4): 207

Abstract: The syntheses and HPLC analysis of N-desmethyltamoxifen and carbon11 labelled tamoxifen are described. In order to obtain the N-desmethyltamoxifen, tamoxifen citrate was first converted to tamoxifen free base. N-desmethyltamoxifen was prepared by reacting tamoxifen free base with 1-chloroethyl-chloroformate(ACE.C). For 12C labeling, N-desmethyltamoxifen was heated with 11C methyl iodide for 10min at 130℃, and the 11C labelled compound was purified by HPLC on a pBonapak TM Cy column. Injectable 11C-tamoxifen was obtained within 50~60 min from EOB (end-of-bombardment) with a labeling yield of 60%-70%.

Key words: Tamoxifen citrate, N-desmethyltamoxifen, 11C-tamoxifen, HPLC